The shikimate pathway for aromatic biosynthesis presents a target for antimalarial drug development as this pathway is absent from animals. This study extends previous work on inhibitors of the shikimate pathway, by examining their interaction with the antimalarial drugs pyrimethamine and atovaquone. Combinations of atovaquone with several shikimate analogues exhibited synergistic effects. Thes...

Abstract: A new series of plasmepsin II (PM II) inhibitors has been prepared based on 4-aminopiperidine-tert-butyl-carbamate (1). These compounds might be useful as antimalarial drugs acting via a new mechanism, and therefore be less susceptible to parasite resistance now often observed with current antimalarial therapies. Some of the final compounds prepared exhibited encouraging inhibitory ac...

Synthesis of novel aminoquinoline derivatives has been accomplished and their activity against malaria strains examined. The compounds showed moderate in vitro antimalarial two P. falciparum strains, 3D7 (CQ susceptible clone) Dd2 resistant clone). Three aminoquinolines were further examined for efficacy a mouse model using modified Thompson test. In this model, mice infected with berghei-infec...

Aim of this study was to standardize the Antimalarial drug sensitivity testing using microtitre plate method similar to WHO III plate method. The study was conducted over a period of two years from January 2013 to December 2014. Total 44 patient samples were included in this study (22 were P. falciparum and 22 were P. vivax). 68.18% of P. falciparum blood samples showed resistance to chloroquin...

BACKGROUND Many acute and chronic neurological sequelae from the quinoline derivative antimalarial drug mefloquine, including dizziness and effects on the visual system such as diplopia and blurred vision, may be attributable to focal central nervous system toxicity. Maculopathy has also been reported with use of mefloquine, although the mechanism of this effect has remained unclear. Identifica...

Several endoperoxide compounds are very efficient antimalarial analogues of the natural drug artemisinin. Quantum chemical calculations have been used to correlate the computed free energies of the O-O bond with respect to the total number of oxygen atoms contained in the cycle, and with the size/strain of the cycle (5- or 6-membered cycles). The gas-phase homolysis of the O-O bond has been stu...